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Ningetinib (CT-053) (CT053PTSA) is an orally bioavailable tyrosine kinase inhibitor with IC50s of <1.0, 1.9 and 6.7 nM for Axl, VEGFR2, and c-Met, respectively.

| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 2 mg | $42 | In Stock | |
| 5 mg | $68 | In Stock | |
| 10 mg | $97 | In Stock | |
| 25 mg | $198 | In Stock | |
| 50 mg | $343 | In Stock | |
| 100 mg | $587 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $75 | In Stock |
| Description | Ningetinib (CT-053) (CT053PTSA) is an orally bioavailable tyrosine kinase inhibitor with IC50s of <1.0, 1.9 and 6.7 nM for Axl, VEGFR2, and c-Met, respectively. |
| Targets&IC50 | VEGFR2:1.9 nM (cell free), Axl:<1 nM (cell free), c-Met:6.7 nM (cell free) |
| In vitro | In cell-based functional assays, Ningetinib inhibits VEGF and HGF-stimulated HUVEC proliferation and microvascular angiogenesis in rat aortic rings with IC50 values of 6.3 and 8.6 nM, respectively. |
| In vivo | In the orthotopic U87MG human glioblastoma xenograft model, Ningetinib prolongs the median survival time and yields a significant increase in life-span value (ILS=32%) at an oral dose of 20 mg/kg/day (dosed 21 days) versus the vehicle-treated group. When single dosed orally (3 mg/kg) to U87MG tumor-bearing nude mice, Ningetinib potently inhibits the phosphorylation of c-Met and its downstream signaling kinases AKT and ERK1/2 for up to 6 hours in tumor tissues. |
| Synonyms | CT053PTSA, CT-053 |
| Molecular Weight | 556.58 |
| Formula | C31H29FN4O5 |
| Cas No. | 1394820-69-9 |
| Smiles | Cc1c(C(=O)Nc2ccc(Oc3ccnc4cc(OCC(C)(C)O)ccc34)c(F)c2)c(=O)n(-c2ccccc2)n1C |
| Relative Density. | 1.348 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||
| Solubility Information | DMSO: 15 mg/mL (26.95 mM), Sonication is recommended. | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
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